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Drug-Target Interaction

Drug

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PubChem ID:5311
Structure:
Synonyms:
149647-78-9
1zz1
4-Dimethylamino-N-(6-hydroxycarbamoylhexyl)benzamide
AC-1923
AC1L1K2K
AIDS-186714
AIDS186714
BRD-K81418486-001-10-3
C111237
CCRIS 8456
CHEBI:45716
CHEMBL98
D06320
DB02546
EC-000.2057
FT-0082592
HMS2219L20
HMS3264D20
LS-186548
LS-186997
LS-187780
M344
M344 compound
MK-0683
MK0683
MLS001065855
N'-hydroxy-N-phenyloctanediamide
N-Hydroxy-7-(4-dimethylaminobenzoyl)aminoheptanamide
N-Hydroxy-N'-phenyl octanediamide
N-hydroxy-N'-phenyl-octane-1,8-diotic acid diamide
N-hydroxy-N'-phenyloctanediamide
N-Hyrdroxy-N'-phenyloctanediamide
N1-hydroxy-N8-phenyloctanediamide
NCGC00168085-01
NCGC00168085-02
NCGC00168085-03
NCGC00168085-04
nchembio.275-comp2
nchembio.313-comp1
nchembio815-comp18
NHNPODA
NSC-701852
NSC701852
Octanediamide, N-hydroxy-N'-phenyl-
OCTANEDIOIC ACID HYDROXYAMIDE PHENYLAMIDE
P111011
S1047_Selleck
SAHA
SAHA cpd
SAHA, Suberoylanilide hydroxamic acid
SHH
SKI390
SMR000486344
Suberanilohydroxamic acid
Suberoylanilide hydroxamic acid
Suberoylanilide hydroxamic acid (SAHA)
SW-064652
UNII-58IFB293JI
Vorinostat
Vorinostat (JAN/USAN)
Vorinostat (USAN)
Vorinostat MSD
Vorinostat [USAN]
Vorinostat-Supplied by Selleck Chemicals
WIN64652
ZINC01543873
Zolinza
Zolinza (TN)
Zolinza, MK-0683, SAHA
ATC-Codes:

Target

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Uniprot ID:Q7KTS4_DROME
Synonyms:
Hdac3
LD23745p
EC-Numbers:3.5.1.-
Organism:Drosophila melanogaster
Fruit fly
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

18413790
MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo.. Marielle Fournel; Claire Bonfils; Yu Hou; Pu Theresa Yan; Marie-Claude Trachy-Bourget; Ann Kalita; Jianhong Liu; Ai-Hua Lu; Nancy Z Zhou; Marie-France Robert; Jeffrey Gillespie; James J Wang; Hélène Ste-Croix; Jubrail Rahil; Sylvain Lefebvre; Oscar Moradei; Daniel Delorme; A Robert Macleod; Jeffrey M Besterman; Zuomei Li (2008) Molecular cancer therapeutics display abstract
Nonselective inhibitors of human histone deacetylases (HDAC) are known to have antitumor activity in mice in vivo, and several of them are under clinical investigation. The first of these, Vorinostat (SAHA), has been approved for treatment of cutaneous T-cell lymphoma. Questions remain concerning which HDAC isotype(s) are the best to target for anticancer activity and whether increased efficacy and safety will result with an isotype-selective HDAC inhibitor. We have developed an isotype-selective HDAC inhibitor, MGCD0103, which potently targets human HDAC1 but also has inhibitory activity against HDAC2, HDAC3, and HDAC11 in vitro. In intact cells, MGCD0103 inhibited only a fraction of the total HDAC activity and showed long-lasting inhibitory activity even upon drug removal. MGCD0103 induced hyperacetylation of histones, selectively induced apoptosis, and caused cell cycle blockade in various human cancer cell lines in a dose-dependent manner. MGCD0103 exhibited potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro, and HDAC inhibitory activity was required for these effects. In vivo, MGCD0103 significantly inhibited growth of human tumor xenografts in nude mice in a dose-dependent manner and the antitumor activity correlated with induction of histone acetylation in tumors. Our findings suggest that the isotype-selective HDAC inhibition by MGCD0103 is sufficient for antitumor activity in vivo and that further clinical investigation is warranted.